Certain pharmaceutical products such as painkillers and decongestants contain “active pharmaceutical ingredients” (API) that can offer a basis for illicit use including, but not limited to, abuse and diversion, such as ingredients providing a profound hallucinogenic effect, or precursors used in the production of drugs (e.g., narcotics). In addition, illicit use can occur with regard to ingredients that can be sold for profit in the illicit market. Among these active pharmaceutical ingredients are, for example, alkaloids such as ephedrine, pseudoephedrine, phenyl propanol amine, opiates such as oxycodone, morphine, hydrocodone, oxymorphone, and the like.
These active pharmaceutical ingredients require high levels of purification and are typically produced from plant extracts using sophisticated and expensive separation (e.g., extraction) technologies and chemical conversions that are available only to a select number of chemical and pharmaceutical companies. Their production is highly controlled by governmental agencies worldwide. However, clandestine efforts to produce these active pharmaceutical ingredients for illicit purposes (e.g., non-medical use) are a major problem and remain the focus of drug enforcement agencies.
Home-based production of these API in high quality directly from plant extracts is extremely difficult because of the sophisticated and expensive equipment required. However, their separation from commercially available pharmaceutical products is relatively simple. Accordingly, efforts are needed to make separation of API from commercial pharmaceutical products more difficult.
A number of API are further classified as “diversion” drugs and “recreational abuse” drugs. Diversion drugs are obtained from an illegal process wherein large quantities of pharmaceutical products containing API are processed to separate the API to make highly potent drugs (e.g., narcotics) for illegal trade. The separation process typically involves dissolving a large quantity of pharmaceutical products such as in the form of tablets in a small volume of a polar solvent, increasing the pH of the solution to precipitate the API, and separating the API with a non-polar solvent for further processing. Increasing the pH typically causes the salt form of the drug to convert to the free base form, which can be extracted by a non-polar solvent such as benzene, toluene, or methyl isobutyl ketone to separate the API from excipients and then utilizing the pure API for further synthesis.
A recreational abuse drug is a personalized use of a pharmaceutical product containing an API by a substance addict for non-medical use. There are several forms of recreational abuse, which include (a) extraction of the API from tablets using dissolution, pH adjustment, and separation for further personal use via intravenous injection, (b) multiple use of several dosage forms to increase the potency of a single application (overdose), and (c) crushing the tablets and inhaling the resulting powder (i.e., snorting) to bypass the digestive system and significantly increase the bioavailability of the API. Making API-containing pharmaceutical products diversion- and/or abuse-resistant is of critical importance to fighting the drug abuse epidemic.
It is desirable to formulate pharmaceutical products containing API in a manner in which the API becomes diversion-resistant (i.e., difficult to separate from the product by conventional means) and/or abuse-resistant (i.e., difficult to administer for a non-therapeutic or non-medical effect). There have been several attempts to formulate diversion- and/or abuse-resistant drugs. In general, these attempts are primarily directed towards developing drugs with a prolonged dissolution profile or include agents such as agonists, irritants, and gel forming compounds, which make it difficult to separate the API. None of these attempts, however, offer a real solution against diversion and recreational abuse and other illicit uses.
Accordingly, there is a need for diversion- and/or abuse-resistant compositions including pharmaceutical compositions, formulated in a manner that more effectively obstruct or impede illicit use of an active pharmaceutical ingredient (API). There is a further need to provide compositions containing API that hinder illicit use including separation of the API via conventional separation methods, making it difficult if not impossible for the illicit drug trade to isolate, purify and provide API for purposes of drug abuse or illicit drug trade.